VINCA.pptx

Vinca Alkaloids

1. VINCA

2. CONTENTS: SYNONYMS BIOLOGICAL SOURCE GEOGRAPHICAL SOURCE CHEMICAL CONSTITUENTS MECHANISM OF ACTION ISOLATION AND ESTIMATION OF VINCA CHEMICAL TEST USES MARKETED PRODUCTS

3. Synonyms : Vinca rosea , Catharanthus , Periwinkle, Madagascar periwinkle Biological source : Vinca consists of the dried leaves and aerial parts of Catharanthus roseus belongs to the family Apocyanaceae . Geographical source : Vinca is indigenous to Madagascar. Cultivated in India, South Africa , U.S.A. , Europe ,Australia.

4. CHEMICAL CONSTITUENTS: . Majority of them are Indole and Dihydroindole derivatives. . Other alkaloids present in vinca are Ajmalicine , Serpentine , Lochnerine and Tetrahydroalstonine .

5. CHEMISTRY:

6. MOA:

7. ISOLATION: Vinca leaves & herb mixed & extracted with aq:alcoholic acetic acid solution Aq:extract concentrated & residue further extracted with 2% HCl pH adjusted to 4 with NaOH & extracted with benzene pH raised to 7 & again extracted with benzene (to seperate alkaloids) The benzene extract with pH 7 are mixed , concentrated,dried Dissolved in benzene – methylene chloride (65:35)

8. Further subjected to chromatographic fractionation on neutral alumina column with benzene –methylene chloride as eluent(using glidient elution technique) Vinblastine rich fraction are evaporated to dryness to yield vinblastine sulphate which crystallise from alcohol. Further elution of column give vincristine which is dried and crystallised from alcohol.

9. IDENTIFICATION: TLC METHOD-1 •Stationary phase - Silica gel •Mobile phase - Acetonitrile:Benzene (30:70) • Detecting agent - 1% solution of Cerric ammonium sulphate in 85% phosphoric acid • Rf value - 0.39 REFERENCE: Textbook of pharmacognosy & phytochemistry by Biren shah & A.K.Seth

10. ESTIMATION OF VINCA: • A simple reversed-phase liquid chromatographic method . •Developed for the simultaneous quantitation of the anticancerous drugs vincristine, vinblastine, and their precursors catharanthine and vindoline . •By using a Merck Chromolith Performance reversed-phase high-performance liquid chromatography column. • A better resolution is obtained in comparison with available particulate-type C18 columns. • Chromatography is carried isocratically with a mobile phase of acetonitrile- 0.1M phosphate buffer containing 0.5% glacial acetic acid ( 21:79, v/v; pH 3.5 ) • A flow rate of 1.2 mL/min and UV detection at 254 nm. REFERENCE: https://www.ncbi.nlm.nih.gov › pubmed

11. CHEMICAL TEST: USES: >Vincristine sulphate is used for acute lymphoid leukemia,small cell lung cancer,cervical & breast cancer >Vinblastine sulphate used in the treatment of carcinoma like Testicular carcinoma in combination with cis platin . >Treatment of Hodgkin’s & non-Hodgkin’s lymphoma. > Vinca exhibits hypotensive & antidiabetic actions. >Administered with Bleomycin & Cis platin for the treatment of metastatic testicular carcinoma. >Treatment of acute leukemia in children.

12. There are four major vinca alkaloids in clinical use: Vinblastine (VBL), vinorelbine (VRL), vincristine (VCR) and vindesine (VDS). VCR, VBL and VRL have been approved for use in the United States. Vinflunine ( A novel drug, which is a fluorinated derivative of vinorelbine) , also a new synthetic vinca alkaloid, which has been approved in Europe for the treatment of second-line transitional cell carcinoma of the urothelium is being developed for other malignancies. Vinca alkaloids are the second-most-used class of cancer drugs and will stay among the original cancer therapies

13. MARKETED PRODUCTS: DRUG TREATMENT DOSAGE Vinca rosea herbal tincture Childhood leukemia,Hodgkin’s disease 1-2 ml/ 3 times daily 2.Vincristine liposomal Brand:MARQIBO Acute lymphoblastic leukemia 0.16mg/ml ( i.v. ) 3.Vinorelbine Brand:NAVELBINE Non-small cell lung cancer .10mg/ml .50mg/ml ( i.v. ) 4.Vinblastine Brand:VELBAN Testicular cancer,Hodgkin’s disease .1mg/ml( i.v. ) .10mg(powder inj.) 5.Oncovin Brand: VINCRISTINE SULPHATE Blood disorders,Acute leukemia i.v. or infusion